1. Anti-infection GPCR/G Protein
  2. HIV Endothelin Receptor
  3. Schisantherin D

Schisantherin D is a lignan. Schisantherin D can be isolated from Kadsura interior. Schisantherin D downregulates the expression of ETBR and inhibits the secretion of ECM and ET-1. Schisantherin D alleviates EtOH + ET-1-induced hepatocyte cytotoxicity. Schisantherin D potently inhibits HIV replication in cells.

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Schisantherin D

Schisantherin D Chemical Structure

CAS No. : 64917-82-4

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Description

Schisantherin D is a lignan. Schisantherin D can be isolated from Kadsura interior. Schisantherin D downregulates the expression of ETBR and inhibits the secretion of ECM and ET-1. Schisantherin D alleviates EtOH + ET-1-induced hepatocyte cytotoxicity. Schisantherin D potently inhibits HIV replication in cells[1][2].

IC50 & Target[1]

ETB

 

Cellular Effect
Cell Line Type Value Description References
H9 EC50
0.5 μg/mL
Compound: 4
Cytotoxicity against mock-infected human H9 cells after 4 days
Cytotoxicity against mock-infected human H9 cells after 4 days
[PMID: 8946749]
H9 IC50
25.3 μg/mL
Compound: 4
Antiviral activity against HIV1 3B in human H9 cells assessed as inhibition of p24 antigen production after 4 days by ELISA
Antiviral activity against HIV1 3B in human H9 cells assessed as inhibition of p24 antigen production after 4 days by ELISA
[PMID: 8946749]
In Vitro

Schisantherin D (50 μM; 2 h) attenuates EtOH + ET-1-induced cytotoxicity and enhances cell viability in HL-7702 hepatocytes[1].
Schisantherin D inhibits the secretion of Col-I, Col-III, FN and ET-1 by LX-2 hepatic stellate cells stimulated with EtOH + ET-1[1].
Schisantherin D (0.8-100 µg/mL; 4 days) potently inhibits HIV replication in H9 lymphocytes, with an EC50 of 0.5 µg/mL, a therapeutic index of 50.6, and a cytotoxic IC50 of 25.3 µg/mL[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: HL-7702 human liver parenchymal cells
Concentration: 50 μM
Incubation Time: 2 h pre-incubation, followed by 24 h co-incubation with EtOH + ET-1
Result: Increased the viability of EtOH + ET-1-injured HL-7702 cells to 90.46%, compared to 77.60% viability in the untreated injury model group.
Showed no cytotoxicity alone, with 94.82% cell viability relative to untreated controls.
Molecular Weight

520.53

Formula

C29H28O9

CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

COC1=C(C([C@@H]([C@@](O)2C)OC(C3=CC=CC=C3)=O)=CC4=C1OCO4)C(C(C[C@@H]2C)=CC5=C6OCO5)=C6OC

Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (192.11 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9211 mL 9.6056 mL 19.2112 mL
5 mM 0.3842 mL 1.9211 mL 3.8422 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (4.80 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.66%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9211 mL 9.6056 mL 19.2112 mL 48.0280 mL
5 mM 0.3842 mL 1.9211 mL 3.8422 mL 9.6056 mL
10 mM 0.1921 mL 0.9606 mL 1.9211 mL 4.8028 mL
15 mM 0.1281 mL 0.6404 mL 1.2807 mL 3.2019 mL
20 mM 0.0961 mL 0.4803 mL 0.9606 mL 2.4014 mL
25 mM 0.0768 mL 0.3842 mL 0.7684 mL 1.9211 mL
30 mM 0.0640 mL 0.3202 mL 0.6404 mL 1.6009 mL
40 mM 0.0480 mL 0.2401 mL 0.4803 mL 1.2007 mL
50 mM 0.0384 mL 0.1921 mL 0.3842 mL 0.9606 mL
60 mM 0.0320 mL 0.1601 mL 0.3202 mL 0.8005 mL
80 mM 0.0240 mL 0.1201 mL 0.2401 mL 0.6003 mL
100 mM 0.0192 mL 0.0961 mL 0.1921 mL 0.4803 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Schisantherin D
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HY-N7543
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